Antagonism of Quorum Sensing Phenotypes by Analogs of the Marine Bacterial Secondary Metabolite 3-Methyl- N-(2'-Phenylethyl)-Butyramide

Mar Drugs. 2019 Jul 1;17(7):389. doi: 10.3390/md17070389.

Abstract

Quorum sensing (QS) antagonists have been proposed as novel therapeutic agents to combat bacterial infections. We previously reported that the secondary metabolite 3-methyl-N-(2'-phenylethyl)-butyramide, produced by a marine bacterium identified as Halobacillus salinus, inhibits QS controlled phenotypes in multiple Gram-negative reporter strains. Here we report that N-phenethyl hexanamide, a structurally-related compound produced by the marine bacterium Vibrio neptunius, similarly demonstrates QS inhibitory properties. To more fully explore structure-activity relationships within this new class of QS inhibitors, a panel of twenty analogs was synthesized and biologically evaluated. Several compounds were identified with increased attenuation of QS-regulated phenotypes, most notably N-(4-fluorophenyl)-3-phenylpropanamide against the marine pathogen Vibrio harveyi (IC50 = 1.1 µM). These findings support the opportunity to further develop substituted phenethylamides as QS inhibitors.

Keywords: Vibrio; phenethylamide; quorum sensing.

MeSH terms

  • Amides / chemistry
  • Amides / metabolism
  • Amides / pharmacology*
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / metabolism
  • Anti-Bacterial Agents / pharmacology*
  • Halobacillus / metabolism*
  • Inhibitory Concentration 50
  • Quorum Sensing / drug effects*
  • Secondary Metabolism
  • Structure-Activity Relationship
  • Vibrio / drug effects
  • Vibrio / physiology

Substances

  • Amides
  • Anti-Bacterial Agents

Supplementary concepts

  • Halobacillus salinus
  • Vibrio harveyi